A series of 2-[(40 -oxo-30 -chloro-20 -phenylazetidin-10 -ylamino)-methyl]-3-[N-isonicotinamide-yl]-quinazolin-4-one hybrids were synthesized starting from anthranilic acid in basic media using chloroacetyl chloride and benzene as solvent. The structure of the synthesized compounds has been evaluated on the basis of their elemental (C, H, and N) and spectral analysis (IR, 1 H NMR, and 13C NMR spectrometry). In vitro antimicrobial evaluation of the synthesized compounds revealed that they posses promising antimicrobial activity against some gram-positive and gram-negative bacteria. Furthermore, compounds 7d and 7f exhibited potent antitubercular activity.